Table 2.
Summary of ex vivo occupancies in the rat and in vitro binding affinities of vortioxetine
| Target | Ex vivo occupancy in the rat ED50 (mg·kg−1) [95% CI] | In vitro binding affinity, Ki (nM) | |
|---|---|---|---|
| Rat | Human | ||
| 5-HT3 | 0.004 [0.0016–0.011] | 1.1 | 3.7 |
| 5-HT7 | NC | 190 | 19 |
| 5-HT1D | ND | 3.7 | 54 |
| 5-HT1B | 2.3 [1.7–3.2] | 16 | 33 |
| 5-HT1A | NC | 230 | 15 |
| SERT | 0.3 [0.24–0.37] | 8.6 | 1.6 |
The ex vivo occupancy ED50 values in the rat were derived based on occupancy–dose curves of vortioxetine for the 5-HT3, 5-HT7, 5-HT1B, 5-HT1A receptors and the SERT as shown in Figure 1. The previously published in vitro binding affinities (Bang-Andersen et al., 2011; Mørk et al., 2012) are also shown in order to highlight the species differences for some of the targets. NC, not calculated due to limited range; ND, not determined.